3-deazaneplanocin A (DZNeP) HCl

Catalog No.S7120 Synonyms: NSC 617989 HCl

3-deazaneplanocin A (DZNeP) HCl Chemical Structure

Molecular Weight(MW): 298.73

3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay.

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Biological Activity

Description 3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay.
Features Carbocyclic analog of adenosine, and acts as anti-tumor and anti-virus inhibitor of EZH2.
Targets
S-adenosylhomocysteine hydrolase [1]
()
50 pM(Ki)
In vitro

3-Deazaneplanocin A (1.0 μM) results in a significant increase in accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G2/M phases (6.3%) of the cell cycle of human acute myeloid leukemia OCI-AML3 cells. 3-Deazaneplanocin A (1.0 μM) induces apoptosis in OCI-AML3 (~50%) and HL-60 cells (~50%), and a more than 90% reduction in colony growth at 48 hr. 3-Deazaneplanocin A depletes EZH2 levels, and inhibits trimethylation of lysine 27 on histone H3 in the HL-60 and OCI-AML3 cells and in primary AML cells. 3-Deazaneplanocin A treatment induces p16, p21, p27, and FBXO32 while depleting cyclin E and HOXA9 levels. 500 nM 3-Deazaneplanocin A induces differentiation of HL-60 to CD11b+ cell by nearly 3-folds time at 48 h. [2] 3-Deazaneplanocin A has excellent activity against several viral types. 3-Deazaneplanocin A is activity against vesicular stomatitis in L929 cells, parainfluenza 3 in H.Ep-2, vaccinia and yellow fever viruses in vero cells with IC50 of 0.2, 3.6, 2.1 and 2.9 μg/mL, respectively. [3] 3-Deazaneplanocin A displays a strongly and uniformly leishmanistatic effect on American Leishmania (L mexicana and L brasiliensis) strains in the study with average ID50 of 96 ng/mL, but shows no inhibition against the several T. cruzi and T. rangeli strains tested with concentrations up to 10 μg/mL. At a dose of 200 ng/mL, 3-Deazaneplanocin A inhibits S-adenosyl-L-3H-methylmethionine and 3-thymidine incorporation by promastigotes after four days. At a dose of 100 ng/mL, 3-Deazaneplanocin A eliminates approximately 56% of the L mexicana and L brasiliensis from infected human macrophages. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HCT116 cells NWTHNYFnS3m2b4TvfIlkyqCjc4PhfS=> MUC3NkBp MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgO|IhcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFnDOVA:OC5{NjFOwG0v NGLKUpUzPjBzMEW4OS=>
human MDA-MB-231 cells M1PrXWN6fG:2b4jpZ:Kh[XO|YYm= MUK3NkBp NHnzfGNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F697zOIFnDOVA:OC5|IN88UU4> NITZUnUzPjBzMEW4OS=>
human SKHEP1 cells MXzDfZRwfG:6aXRCpIF{e2G7 M3jNTFczKGh? M1jGNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMUEWSMTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA4OiCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygTWM2OD1yLkeyJO69VS5? MlrGNlYxOTB3OEW=
human SNU638 cells MV7DfZRwfG:6aXRCpIF{e2G7 NVu1WFZRPzJiaB?= MkTrR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25WPjN6IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxRTBwOUGg{txONg>? NVj5UnIyOjZyMUC1PFU>
human A549 cells NF3I[pNEgXSxdH;4bYPDqGG|c3H5 M1;IbVczKGh? MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwQVEvPCEQvF2u M3TZc|I3ODFyNUi1
human PC3 cells Mmr0R5l1d3SxeHnjxsBie3OjeR?= NYCyR|g{PzJiaB?= NVXpSmYzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDJR|UxRTlwM{mg{txONg>? NFP5PYUzPjBzMEW4OS=>

... Click to View More Cell Line Experimental Data

In vivo 3-Deazaneplanocin A shows antileukemia activity in vivo. 3-Deazaneplanocin A (1 mg/kg) significantly prolongs survival of mice implanted with AML cells with a median survival of 43 days compared with control group (36 days), which can be further improved by co-treatment with 10 mg/kg pan-HDAC inhibitor (HDI) panobinostat (52 days, median survival). [2] 3-Deazaneplanocin A at the doses of 8 mg/kg shows in vivo antiviral activity against vaccinia virus in a mouse tailpox assay with median of 0.0 poxftail (84% protection). [3] 3-Deazaneplanocin A at the doses ranging from 0.5 to 1.5 mg/kg/day, significantly reduced development of cutaneous leishmanial infection produced in inbred BALB/c mice by L. b. guyanensis inoculation. [4] 3-Deazaneplanocin A induces massively increased interferon-α production in Ebola virus-infected mice. 3-Deazaneplanocin A (s.c. injection of 2 mg/kg postinfection) prevents death in mice infected with 1000 pfu (30 000 LD50) of mouse-adapted EBO-Z. Treatment with 3-Deazaneplanocin A on day 1 reduces mean serum viral titers on day 2 by 100-fold and on day 3 by 100 000-fold, compared with placebo controls, and results in a mean serum IFN-α level of 1420 pg/mL on day 2 and 1830 pg/mL on day 3. [5]

Protocol

Kinase Assay:

[6]

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S-adenosylhomocysteine hydrolase activity assay:

The reaction mixture used for assay of AdoHcyase contains, in a final volume of 0.5 mL, 50 mM potassium phosphate (pH 7.6), 5 mM dithiothreitol, 1 mM EDTA, 10% glycerol, and the enzyme. L-[8- 14C]AdoHcy is used as substrate and 5 units of calf intestinal adenosine deaminase are included. The reaction is stopped by the addition of 100 μL of 5 M formic acid, and the reaction mixture is then poured onto a column (0.8×2.5 cm) of SP-Sephadex C-25, previously equilibrated in 0.1 M formic acid. Each test tube is rinsed with 0.5 mL of 0.1 M formic acid. [14C]Inosine formed is eluted from the column by 3.5 mL of 0.1 M formic acid into a scintillation vial. The radioactivity is determined after the addition of 10 mL of scintillation fluid. The amount of enzyme used is about 105 pU, or 75 ng of the purified enzyme. One unit is the amount of enzyme needed to form 1 pmol of product in 1 min at 37 ℃.
Cell Research:

[2]

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  • Cell lines: Human acute myeloid leukemia HL-60
  • Concentrations: ~1 μM
  • Incubation Time: 2 days
  • Method:

    Cells are treated with the indicated concentrations of 3-Deazaneplanocin A for 48 hours. After the designated treatments, cells are harvested and washed twice with PBS, and approximately 500 cells are plated in complete Methocult and cultured for 7 to 10 days at 37 ℃ in a 5% CO2 environment. Cells are dyed with crystal violet, and relative colony density is determined by solubilizing the crystal violet dye in 10% acetic acid followed by measurement of absorbance at 450 nm.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Human acute myeloid leukemia xenografts HL-60
  • Formulation: --
  • Dosages: 1 mg/kg
  • Administration: initiated on day 7 and administered twice per week (Tuesday-Thursday) intraperitoneally for 2 weeks
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 52 mg/mL (174.07 mM)
Water 52 mg/mL (174.07 mM)
Ethanol Insoluble
In vivo Add solvents individually and in order:
Saline
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 298.73
Formula

C12H14N4O3.HCl

CAS No. 120964-45-6
Storage powder
Synonyms NSC 617989 HCl

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID